PB28 dihydrochloride | Potent sigma2 agonist

PB28 (172907-03-8) is a very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) σ2 agonist.  Selective for σ2 over σ1 (approx 30-40x).1,2 PB28 inhibited cell growth in MCF7 and MCF7 ADR breast cancer cells and displayed strong synergism with doxorubicin.3  PB28 potently inhibited Kv2.1 currents in a σ-independent manner.4 PB28 was recently found to have potent (IC50 = 280 nM) anti-SARS-CoV2 activity.5

References:

  1. Berardi et al. (1996), New s and 5-HT1A Receptor Ligands: w-(Tetralin-1-yl)-n-alkylamine Derivatives; Med. Chem. 39 176
  2. Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as s Receptor Ligands with Agonist s2 Activity; Med. Chem. 47 2308
  3. Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a s2 agonist and s1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclins in breast cancer; Cancer Ther. 5 1807
  4. Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345
  5. Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 459
Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
Size:

5 mg, 25 mg

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CAS:
172907-03-8
Catalog Number:
10-4665
Activity:
High affinity sigma2 ligand
Chemical Names:
1-Cyclohexyl-4-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]piperazine dihydrochloride
Molecular Weight:
443.50
Molecular Formula:
C24H38N2O
Solubility:
Soluble in DMSO (>25 mg/ml) or water (5 mg/ml)
Physical Properties:
White to off-white solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

PB28 dihydrochloride | Potent sigma2 agonist

$45.00$160.00

CAS:
172907-03-8
Catalog Number:
10-4665
Activity:
High affinity sigma2 ligand
Chemical Names:
1-Cyclohexyl-4-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]piperazine dihydrochloride
Molecular Weight:
443.50
Molecular Formula:
C24H38N2O
Solubility:
Soluble in DMSO (>25 mg/ml) or water (5 mg/ml)
Physical Properties:
White to off-white solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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